Cytopia Received Patent for JAK Kinase Inhibitors

Australian-based biotech drug discovery company Cytopia Pty Ltd. has lately received an Indian Patent No. 214081 (the ‘081 patent) for disubstituted pyrazine compounds having protein kinase, particularly Janus kinase (JAK) inhibitory activity. The ‘081 patent is issued against the mail-box application no. 1743/KOLNP/2004 dated November 17, 2004, claiming earliest priority from an Australian provisional application dated May 23, 2002. The published abstract of the Indian application (u/s 11A, the Patents Act, 1970) reads as –

"A compound of the general formula (I) or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states using the compound of formula (I) is also described."

Referring corresponding US Patent No. 7,259,179, the disubstituted pyrazine compounds are used to treat protein kinase-associated disorders which result from aberrant protein kinase activity, in particular JAK activity and/or which are alleviated by inhibition of one or more of these enzymes. Further referring that the term ‘JAK’, ‘JAK kinase’ or ‘JAK family’ refers to protein tyrosine kinases which posses characterizing features of JAK1, JAK2, and JAK3.

Cytopia has few other pending applications with Indian Patent Office for drug targets in same class of JAK inhibitors to treat immune diseases and cancer.

1. 1748/KOLNP/2004 – Protein Kinase Inhibitors
2. 845/KOLNP/2006 – Selective Kinase Inhibitors
3. 616/KOLNP/2006 - Azole-based Kinase Inhibitors

In June 2006, Cytopia signed a licensing deal with Novartis to develop JAK3 inhibitor compounds for the prevention of transplant rejection and the treatment of multiple indications of autoimmune diseases. Under the deal Novartis will pay Cytopia approximately $ 9.5 million over three years including an up front payment and research funding. Over the life of deal Cytopia may also become eligible to receive development, regulatory and sales milestones which could total approximately US $ 205 million if an agreed number of multiple indications are successfully commercialized. Cytopia will also receive royalties on product sales.

Cytopia lately announced that its lead JAK2 inhibitor compound CYT387 demonstrated potent activity in cells isolated from patients with myeloproliferative disorders (MPDs). Till date, none of Cytopia’s JAK inhibitors is in any phase of clinical trials, but Cytopia’s anti-cancer lead drug CYT997 has already received IND status by the US FDA and likely to reach phase II trials. CYT997 belongs to class of cancer drugs known as Vascular Targeting Agents (VTAs) and is modified version of another compound CYT490. The application no. 847/KOLNP/2006 for CYT997 is pending with Kolkata Patent Office and was published in the Patent Office Journal in April last year.